Novel 3-azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity

…, T Stauder, JP Kramb, S Plutizki, T Kindler…

Index: Ganser, Christopher; Lauermann, Eva; Maderer, Annett; Stauder, Torsten; Kramb, Jan-Peter; Plutizki, Stanislav; Kindler, Thomas; Moehler, Markus; Dannhardt, Gerd Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9531 - 9540

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Citation Number: 16

Abstract

Tumor growth and metastasis are highly associated with the overexpression of protein kinases (PKs) regulating cell growth, apoptosis resistance, and prolonged cell survival. This study describes novel azaindolyl-maleimides with significant inhibition of PKs, such as VEGFR, FLT-3, and GSK-3β which are related to carcinogenesis. Furthermore, these compounds exhibit high kinase selectivity and potent inhibition of angiogenesis and cell ...